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Notopterol is a furanocoumarin originally isolated from H. weberbaueriana that has diverse biological activities.1,2,3 It is an inhibitor of JAK2 and JAK3 (IC50s = 9.51 and 25.2 µM, respectively) and is selective for JAK2 and JAK3 over tyrosine kinase 2 (TYK2) and JAK1 (IC50s = >667 and >2,000 µM, respectively).1 Notopterol (40 and 60µM) induces apoptosis and mitochondrial membrane depolarization in HL-60 leukemia cells.2 It induces cell cycle arrest at the G0/G1 phase in HL-60 cells when used at concentrations of 10, 20, and 40 µM. Notopterol (100 mg/kg) decreases acetic acid-induced writhing and vascular permeability in mice.3 It increases the duration of pentobarbital-induced sleep in mice when administered at doses of 10 or 30 mg/kg. In vivo, notopterol (20 mg/kg per day) reduces joint swelling, inhibits collagen-induced decreases in talus bone volume, and reduces the number of meniscus and talus osteoclasts in a mouse model of collagen-induced arthritis.1
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1. The natural compound notopterol binds and targets JAK2/3 to ameliorate inflammation and arthritis. Cell Rep. 32(11), 108158 (2020).
2. Notopterol-
3. Analgesic component of Notopterygium incisum Ting. Chem. Pharm. Bull. (Tokyo) 41(5), 926-929 (1993).